PMID- 36168148
OWN - NLM
STAT- MEDLINE
DCOM- 20230103
LR  - 20230413
IS  - 2160-7648 (Electronic)
IS  - 2160-763X (Print)
IS  - 2160-763X (Linking)
VI  - 12
IP  - 1
DP  - 2023 Jan
TI  - Pharmacokinetics, Bioavailability, and Swallowing Safety With Riluzole Oral Film.
PG  - 57-64
LID - 10.1002/cpdd.1168 [doi]
AB  - Dysphagia is highly prevalent in patients with amyotrophic lateral sclerosis 
      (ALS). Riluzole is a US Food and Drug Administration-approved treatment for ALS. 
      Riluzole oral film (ROF; Exservan) contains riluzole in a polymer-based film 
      matrix. The ROF is administered by placing on the tongue, where it dissolves and 
      the drug is ingested with the saliva. Two clinical trials assessed the safety and 
      tolerability of the ROF. Bioavailability and pharmacokinetics (PK) were evaluated 
      in an open-label, randomized, single-dose, replicate crossover study of 50 mg of 
      ROF and riluzole 50-mg tablets in 32 healthy volunteers. The second study was a 
      videofluoroscopic swallowing examination conducted with nine patients with ALS 
      before and after receiving a single dose of 50 mg of ROF. The primary outcome was 
      change on penetration-aspiration scale (PAS) scores from pre- to post-dose. 
      Overall, the PK parameters for ROF and riluzole tablets were comparable between 
      treatments and administrations when administered under fasting conditions. 
      Administration of ROF with food resulted in a 15% reduction in area under the 
      curve and a 45% reduction in maximum serum concentration. A total of 44 
      treatment-emergent adverse events (AEs) were reported in the study; all were mild 
      in severity. No serious AEs were observed and no subjects discontinued due to 
      AEs. In the swallowing study, very little numerical or categorical change was 
      observed following the dose of ROF. No evidence of deterioration of swallowing 
      function was observed post-dose. The ROF was bioequivalent to riluzole tablets, 
      was well tolerated, and had no detrimental effect on swallowing.
CI  - (c) 2022 The Authors. Clinical Pharmacology in Drug Development published by Wiley 
      Periodicals LLC on behalf of American College of Clinical Pharmacology.
FAU - Wymer, James
AU  - Wymer J
AD  - University of Florida, Gainesville, Florida, USA.
FAU - Apple, Stephen
AU  - Apple S
AD  - Mitsubishi Tanabe Pharma America, Inc., Jersey City, New Jersey, USA.
FAU - Harrison, Antoinette
AU  - Harrison A
AD  - Mitsubishi Tanabe Pharma America, Inc., Jersey City, New Jersey, USA.
FAU - Hill, Bryan Alan
AU  - Hill BA
AD  - Mitsubishi Tanabe Pharma America, Inc., Jersey City, New Jersey, USA.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20220927
PL  - United States
TA  - Clin Pharmacol Drug Dev
JT  - Clinical pharmacology in drug development
JID - 101572899
RN  - 7LJ087RS6F (Riluzole)
SB  - IM
MH  - United States
MH  - Humans
MH  - *Riluzole/adverse effects
MH  - *Amyotrophic Lateral Sclerosis/drug therapy/chemically induced
MH  - Biological Availability
MH  - Deglutition
MH  - Cross-Over Studies
PMC - PMC10087659
OTO - NOTNLM
OT  - Amyotrophic Lateral Sclerosis
OT  - Clinical Trials
OT  - Drug Development
OT  - Drug-food Interactions
OT  - Dysphagia
OT  - Neurology
OT  - Pharmacokinetics and Drug Metabolism
OT  - Riluzole
OT  - Swallow
EDAT- 2022/09/29 06:00
MHDA- 2023/01/04 06:00
PMCR- 2023/04/11
CRDT- 2022/09/28 00:33
PHST- 2022/05/27 00:00 [received]
PHST- 2022/08/15 00:00 [accepted]
PHST- 2022/09/29 06:00 [pubmed]
PHST- 2023/01/04 06:00 [medline]
PHST- 2022/09/28 00:33 [entrez]
PHST- 2023/04/11 00:00 [pmc-release]
AID - CPDD1168 [pii]
AID - 10.1002/cpdd.1168 [doi]
PST - ppublish
SO  - Clin Pharmacol Drug Dev. 2023 Jan;12(1):57-64. doi: 10.1002/cpdd.1168. Epub 2022 
      Sep 27.